The (un)targeted cancer kinome

被引：228

作者：

Fedorov, Oleg ^{[1
]}

Mueller, Susanne ^{[1
]}

Knapp, Stefan ^{[1
,2
]}

机构：

[1] Univ Oxford, Nuffield Dept Clin Med, Struct Genom Consortium, Oxford, England

[2] Univ Oxford, Dept Clin Pharmacol, Oxford, England

来源：

NATURE CHEMICAL BIOLOGY | 2010年 / 6卷 / 03期

关键词：

MOLECULE KINASE INHIBITORS; DRUG DISCOVERY; COLORECTAL CANCERS; DRIVER MUTATIONS; TYROSINE KINASE; INTERACTION MAP; CELLS; REQUIREMENTS; GENES; SCREEN;

D O I：

10.1038/nchembio.297

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The complexity of cancer signaling and the resulting difficulties in target selection have strongly biased kinase drug discovery towards clinically validated targets. Recently, novel kinase targets that are uncharacterized have emerged from genome sequencing and RNAi studies. Chemical probes are urgently needed to functionally annotate these kinases and to stimulate new drug discovery efforts.

引用

页码：166 / 169

页数：4

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